Abstract: This invention is concerned with mammalian metabolites of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)-phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist that is useful in the prevention and treatment of certain disorders, including emesis and psychiatric disorders such as depression and anxiety.

Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

Abstract: This invention relates to certain 5-HT4 receptor modulators, particularly 5-HT4 receptor antagonists, represented by Formula I: wherein Z is formula (A) or (B): wherein R1, R2, R3, R4, and R5 and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.

Abstract: Disclosed are compounds that are highly selective partial agonists or antagonists at human CRF.sub.1 receptors that are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety. The compounds have the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein Ar, R.sub.1, R.sub.2, A, and Z are various organic and inorganic substituents.

Abstract: N-?4-(cyanoethylthiomethyl)-2-thiazolyl!guanidine--a key intermediate for preparing the pharmaceutical, famotidine--is produced by mixing in a liquid medium formed from a chemically indifferent organic solvent and water, and under an inert atmosphere, (i) a 2-guanidino-4-halomethylthiazole or a hydrohalide complex thereof, (ii) an S-(2-cyanoethyl)isothiourea or a hydrohalide complex thereof, and (iii) a strong alkali metal base. In lieu of (ii), an alkali metal salt of 2-cyanoethyl-1-thiol can be used, and in such case use of (iii) is optional, but preferable.

Abstract: Fungicidally active aminomethyl-isoxazolidines of the ##STR1## in which R.sup.1 represents optionally substituted alkyl, or represents optionally substituted cycloalkyl, or represents optionally substituted tetrahydronaphthyl, or represents optionally substituted decahydronaphthyl andR.sup.2 and R.sup.3 independently of one another each represent hydrogen, or represent in each case optionally substituted alkyl, alkenyl, cycloalkyl or aryl, or together with the nitrogen atom to which they are bonded represent an optionally substituted saturated heterocyclic radical, which can optionally contain further hetero atoms,and acid addition salts thereof. Some intermediates therefor are also new.

Abstract: A novel compound of formula: ##STR1## useful as analgesic and anti-inflammatory drug, with very interesting therapeutic index.

Abstract: The invention provides novel non-toxic biodegradable derivatives of the formula: ##STR1## wherein Ra is (1-12C)alkyl, phenyl, naphthylmethyl or cinnamyl, the aromatic rings of which optionally bear one or two halogeno substituents, or Ra is benzyl optionally bearing up to 3 substituents independently selected from halogeno, trifluoromethyl, (1-4C)alkyl, (1-4C)alkoxy, nitro, cyano and hydroxy; Rb and Rc are independently selected from hydrogen and non-toxic biodegradable protecting radicals, but are not both hydrogen; and benzene ring A optionally bears one substituent selected from halogeno, (1-4C)alkyl, (1-4C)alkoxy, nitro and hydroxy, or bears two substituents independently selected from halogeno, (1-4C)alkyl and nitro; pharmaceutical compositions thereof; and processes for their manufacture.The amides of formula I in which Rb.dbd.Rc.dbd.H are potent inhibitors of the enzyme aldose reductase.